公开(公告)号：EP0947502A4

公开(公告)日：2004-12-01

申请号：EP97939187

申请日：1997-09-05

申请人： SANTEN PHARMA CO LTD

发明人： HORIUCHI MASATO ,  FUJIMURA KENICHI ,  SUHARA HIROSHI

IPC分类号： C07C323/60 ,  C07C323/65 ,  C07C329/06 ,  A61K31/165 ,  A61K31/195 ,  A61K31/215 ,  A61K31/275

CPC分类号： C07C323/65 ,  C07C323/60 ,  C07C329/06 ,  C07C2601/14

摘要： Novel sulfur-containing amino acid derivatives of general formula (I) and exhibiting a high inhibitory activity against LTA4 hydrases. In said formula (I), R is H, alkyl, (substituted) phenylalkyl, alkanoyl or (substituted) benzoyl; R is ester, amide or carboxyl; R is hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, (substituted) phenyl, (substituted) phenoxy, (substituted) phenylthio, halogeno, alkylsulfonyl, halogenoalkylsulfonyl, nitro or cyano; R is alkyl; and A and A are each alkylene.

公开(公告)号：EP1172358A4

公开(公告)日：2003-04-02

申请号：EP00915411

申请日：2000-04-07

申请人： SANTEN PHARMA CO LTD

发明人： MITA SHIRO ,  HORIUCHI MASATO ,  BAN MASAKAZU ,  SUHARA HIROSHI

IPC分类号： A61K31/17 ,  A61P43/00 ,  C07C275/14 ,  C07C275/18 ,  C07C275/24 ,  C07C323/44 ,  C07C327/06 ,  A61K31/22 ,  A61K31/221 ,  A61K31/27

CPC分类号： C07C323/44 ,  A61K31/17 ,  C07C275/14 ,  C07C275/18 ,  C07C275/24 ,  C07C327/06 ,  C07C2601/14

摘要： The N-substituted-N'-substituted urea derivative of formula (a), analogues of the same, or medicinally acceptable salts of both, having a TNF-production inhibiting effect.

摘要翻译： 本文提供了由下式表示的N-取代的N'-取代的脲衍生物，其类似物或其药学上可接受的盐。 这些化合物显示TNF-α产生抑制活性。

公开(公告)号：EP0870762A4

公开(公告)日：2000-03-08

申请号：EP96904324

申请日：1996-03-05

申请人： SANTEN PHARMA CO LTD

发明人： KAWASHIMA YOICHI ,  HORIUCHI MASATO

IPC分类号： C07C323/59 ,  C07C323/60 ,  C07C327/32 ,  A61K31/16 ,  A61K31/19 ,  A61K31/22

CPC分类号： C07C323/60 ,  C07C323/59 ,  C07C327/32

摘要： Novel amino acid derivatives having an N,N-dialkylaminophenyl group represented by general formula (I), wherein R represents hydrogen, lower alkyl, phenyl lower alkyl, lower alkanoyl or benzoyl, provided that the phenyl ring in the phenyl lower alkyl or benzoyl may be substituted by halogeno, lower alkyl or lower alkoxy; R represents carboxyl optionally converted into ester, amide or hydroxamic acid; R represents lower alkyl; R represents lower alkyl; A represents lower alkylene optionally substituted by phenyl, provided that the phenyl group may be substituted by halogeno, lower alkyl or lower alkoxy; A represents lower alkylene; A represents lower alkylene; and Z represents S or O. The compounds have inhibitory effects on LTA and hydrolase and are useful as a drug, in particular, a remedy for diseases in which LTB4 participates such as rheumatism, psoriasis, inflammatory intestinal diseases, gout, cystic fibrosis, etc.

公开(公告)号：EP1103543A4

公开(公告)日：2005-06-22

申请号：EP99935077

申请日：1999-08-04

申请人： SANTEN PHARMA CO LTD

发明人： MITA SHIRO ,  HORIUCHI MASATO ,  BAN MASAKAZU ,  SUHARA HIROSHI

IPC分类号： C07D213/40 ,  C07D233/61 ,  C07D233/64 ,  C07D207/325 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  A61K31/47 ,  A61K31/505 ,  C07D209/16 ,  C07D213/36 ,  C07D215/12 ,  C07D235/16 ,  C07D239/26 ,  C07D409/12

CPC分类号： C07D213/40

摘要： Novel urea derivatives represented by general formula (I) and salts thereof, which exhibit an inhibitory effect against the production of TNF-α and are useful as remedies for various diseases, particularly autoimmune diseases such as rheumatoid arthritis, wherein R1 is H, alkyl, phenyl or formula (II) R2 is H, alkyl, carboxyl, an ester thereof or the like; R?3 and R4¿ are each H, alkyl, cycloalkyl or the like; R5 is H, alkyl, hydroxyl or the like; R6 is a nitrogenous aromatic heterocycle; and A?1 and A2¿ are each alkylene.

公开(公告)号：EP1072591A4

公开(公告)日：2005-01-05

申请号：EP99910724

申请日：1999-03-25

申请人： SANTEN PHARMA CO LTD

发明人： MITA SHIRO ,  HORIUCHI MASATO ,  BAN MASAKAZU ,  SUHARA HIROSHI

IPC分类号： C07C317/50 ,  C07C323/44 ,  C07C323/59 ,  C07C323/60 ,  C07C327/30 ,  C07C329/06 ,  C07D233/61 ,  C07D295/185 ,  C07D333/32 ,  A61K31/17 ,  A61K31/415 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  C07C275/16 ,  C07C275/24 ,  C07C327/22 ,  C07D213/40 ,  C07D295/12 ,  C07D295/18 ,  C07F7/18 ,  A61K31/595

CPC分类号： C07D295/185 ,  C07C317/50 ,  C07C323/44 ,  C07C323/59 ,  C07C323/60 ,  C07C327/30 ,  C07C329/06 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D333/32

摘要： Compounds having a urea structure as the basic structure and carrying sulfur and amide bonds in side chains. It has been found out that these compounds have pharmacological effects, in particular, a TNF-α production inhibitory effect. The above compounds are represented by general formula [I] wherein R1 represents H, alkyl, an aromatic group, R?A-CO-, RC¿-S- or a group of formula [II]; R?2, R3 and R4¿ represent each H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or an aromatic group; R?5 and R6¿ represent each H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or an aromatic group, or R?5 and R6¿ may form together a nonaromatic heterocycle; R7 represents H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, R?B-O-, RC-S-, RD¿-COS-, RE-OCO-, RF-N(RG)- or -CONHOH; and A?1 and A2¿ represent each an alkylene.

公开(公告)号：EP1172359A4

公开(公告)日：2002-09-11

申请号：EP00915410

申请日：2000-04-07

申请人： SANTEN PHARMA CO LTD

发明人： MITA SHIRO ,  HORIUCHI MASATO ,  BAN MASAKAZU ,  SUHARA HIROSHI

IPC分类号： A61K31/4453 ,  A61P37/06 ,  A61P43/00 ,  C07D207/09 ,  C07D211/26 ,  C07D211/46 ,  C07D211/58 ,  C07D211/70 ,  C07D217/04 ,  C07D295/13 ,  A61K31/40 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/695 ,  C07D295/12 ,  C07F7/18

CPC分类号： C07D295/13 ,  A61K31/4453 ,  C07D207/09 ,  C07D211/26 ,  C07D211/46 ,  C07D211/58 ,  C07D211/70 ,  C07D217/04

摘要： The N-substituted-N'-substituted urea derivative of formula (1), analogues of the same, or medicinally acceptable salts of both, having a TNF-α production inhibiting effect.

公开(公告)号：EP0979817A4

公开(公告)日：2001-01-10

申请号：EP98910975

申请日：1998-03-25

申请人： SANTEN PHARMA CO LTD

发明人： MITA SHIRO ,  HORIUCHI MASATO ,  BAN MASAKAZU ,  FUJIMURA KENICHI ,  SUHARA HIROSHI

IPC分类号： A61K31/40 ,  A61K31/401 ,  A61P29/00 ,  A61P43/00 ,  C07D207/16 ,  C12N9/99

CPC分类号： C07D207/16

摘要： Leukotriene A4 hydrolaze inhibitors containing a compound of general formula (I) or a salt thereof as the active ingredient, wherein R1 represents hydrogen, alkyl, phenylalkyl, alkanoyl or benzoyl; R?2 and R3¿ each represent hydrogen or alkyl; R4 represents hydroxyl, alkoxyl, phenylalkoxyl, amino, alkylamino or phenylalkylamino; R5 represents phenylalkyl or naphthylalkyl; Z represents sulfur or oxygen; A represents alkylene; and n represents 0, 1 or 2, provided that the phenyl ring in R1 may be substituted with alkyl, alkoxyl or halogen, and that the phenyl ring or naphthyl ring in R5 may be substituted with alkyl, cycloalkyl, alkoxyl, alkylthio or halogen.